Staurosporine, a microbial alkaloid with antifungal activity, has been shown to inhibit a variety of kinases including PKA (Ki=7.0 nM), PKG (Ki=8.5 nM), MLCK (Ki=1.3 nM), PKC (Ki=0.7 nM), CaMK (ic50 =20 nM)3, CAMKII (Ki=20nM), tyrosine kinases (ic50 = 70 nM) and phosphorylase kinase (ic50 =0.5 nM).

Inhibition is via interaction with the ATP binding site. It induces PKC translocation, induces association of purified PKC with inside-out vesicles from erythrocyte membranes and augments PMA-induced ornithine decarboxylase. Activates a bcl-2-regulated apoptosis pathway.